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533919 Galactokinase Inhibitor, Cpd36 - Calbiochem

A cell-permeable, highly selective inhibitor of galactokinase 1 (GALK1, IC₅₀ = 4.7 µM). The inhibition appears to be competitive with respect to ATP and uncompetitive with respect to galactose.

Galactokinase Inhibitor, Cpd36 - Calbiochem MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: 2-(Benzo[d]oxazol-2-ylamino)-4-(4-chloro-1H-pyrazol-3-yl)-4,6,7,8-tetrahydroquinazolin-5(1H)-one, GALK1 Inhibitor, Cpd36

Primary Target: GALK1
533919
Purchase on Sigma-Aldrich

Áttekintés

Replacement Information

Kulcsspecifikációk táblázata

Empirical Formula
C₁₈H₁₅ClN₆O₂

Products

KatalógusszámCsomagolás Menny./csomag
5.33919.0001 Üvegpalack 10 mg
Description
OverviewA cell-permeable tetrahydroquinazolinone derivative that acts as a highly selective inhibitor of galactokinase 1 (GALK1, IC50 = 4.7 µM in a GALK-ATP depletion assay). The inhibition appears to be competitive with respect to ATP and uncompetitive with respect to galactose. Exhibits higher affinity for GALK1-galactose complex than the free enzyme. Does not affect GALK2 activity even at higher concentrations (~ 40 µM) and has no significant effect on all other protein kinases profiled. Shown to reduce Gal-1-phosphate levels in patient derived fibroblasts without affecting their viability. Displays good plasma (t1/2 >60 min) and microsomal stability (t1/2
Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.
Catalogue Number533919
Brand Family Calbiochem®
Synonyms2-(Benzo[d]oxazol-2-ylamino)-4-(4-chloro-1H-pyrazol-3-yl)-4,6,7,8-tetrahydroquinazolin-5(1H)-one, GALK1 Inhibitor, Cpd36
DescriptionGalactokinase Inhibitor, Cpd36
References
ReferencesLiu, L., et al. 2015. Bioorg. Med. Chem. Lett. 25, 721.
Product Information
FormOff-white solid
Hill FormulaC₁₈H₁₅ClN₆O₂
ReversibleY
Quality LevelMQ100
Applications
Biological Information
Primary TargetGALK1
Purity≥98% by HPLC
Physicochemical Information
Cell permeableY
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
Toxicity Standard Handling
Storage -20°C
Protect from Light Protect from light
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications
Global Trade Item Number
Katalógusszám GTIN
5.33919.0001 04055977281590

Documentation

Galactokinase Inhibitor, Cpd36 - Calbiochem MSDS

Title

Safety Data Sheet (SDS) 

Galactokinase Inhibitor, Cpd36 - Calbiochem Certificates of Analysis

TitleLot Number
533919

References

Hivatkozások áttekintése
Liu, L., et al. 2015. Bioorg. Med. Chem. Lett. 25, 721.
Data Sheet

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision19-November-2016 JSW
Synonyms2-(Benzo[d]oxazol-2-ylamino)-4-(4-chloro-1H-pyrazol-3-yl)-4,6,7,8-tetrahydroquinazolin-5(1H)-one, GALK1 Inhibitor, Cpd36
DescriptionA cell-permeable tetrahydroquinazolinone derivative that acts as a highly selective inhibitor of galactokinase 1 (GALK1, IC50 = 4.7 µM in a GALK-ATP depletion assay). The inhibition appears to be competitive with respect to ATP and uncompetitive with respect to galactose. Exhibits higher affinity for GALK1-galactose complex than the free enzyme. Does not affect GALK2 activity even at higher concentrations (~ 40 µM) and has no significant effect on all other protein kinases profiled. Shown to reduce Gal-1-phosphate levels in patient derived fibroblasts without affecting their viability. Displays good plasma (t1/2 >60 min) and microsomal stability (t1/2
Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.
FormOff-white solid
Intert gas (Yes/No) Packaged under inert gas
Purity≥98% by HPLC
SolubilityDMSO (20 mg/ml)
Storage Protect from light
-20°C
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity Standard Handling
ReferencesLiu, L., et al. 2015. Bioorg. Med. Chem. Lett. 25, 721.